Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening

被引：48
作者：
Holloway, Georgina A.
Baell, Jonathan B.
Fairlamb, Alan H.
Novello, Patrizia M.
Parisot, John P.
Richardson, John
Watson, Keith G.
Street, Ian P.
机构：
[1] Walter & Eliza Hall Inst Med Res, Ctr Biotechnol, Bundoora, Vic 3086, Australia
[2] Univ Dundee, Sch Life Sci, Div Biol Chem & Mol Microbiol, Wellcome Trust Bioctr, Dundee, Scotland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期
基金：
英国惠康基金;
关键词：
tropical diseases; trypanosomiasis therapeutics; trypanothione reductase inhibitors; high-throughput screening; medicinal chemistry; iminobenzimidazoles;
D O I：
10.1016/j.bmcl.2006.11.090
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A high-throughput screening campaign of a library of 100,000 lead-like compounds identified 2-iminobenzimidazoles as a novel class of trypanothione reductase inhibitors. These 2-iminobenzimidazoles display potent trypanocidal activity against Trypanosoma brucei rhodesiense, do not inhibit closely related human glutathione reductase and have low cytotoxicity against mammalian cells. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1422 / 1427
页数：6
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